Catalytic asymmetric Friedländer condensation to construct cyclobutanone-fused quinolines with a quaternary stereogenic centre

Abstract

The first catalytic desymmetric Friedländer condensation of 2-aminobenzophenone with prochiral cyclobutane-1,3-dione has been achieved using chiral phosphoric acid catalysis. A series of cyclobutanone-fused quinolines with quaternary stereogenic centres were obtained in up to 98% yield and 94% ee.